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Assay Detail

CHEMBL2015355

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human CYP11B1 expressed in hamster V79 MZ cells using [3H] 11 deoxycorticosterone as substrate by HPLC radioflow detector
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type V79
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 11B1, mitochondrial (CHEMBL1908)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of the First Selective Steroid-11β-hydroxylase (CYP11B1) Inhibitors for the Treatment of Cortisol Dependent Diseases.
Hille UE, Zimmer C, Haupenthal J, Hartmann RW.
ACS Med Chem Lett (2011) 2 : 559 -564
PubMed 24900349 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 6.81 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL681 ETOMIDATE 4.0 1 9.30
CHEMBL934 METYRAPONE 4.0 1 7.82
CHEMBL2011431 1 7.80
CHEMBL2011246 1 7.77
CHEMBL2011437 1 7.54
CHEMBL2011433 1 7.40
CHEMBL2011253 1 7.38
CHEMBL2011242 1 7.21
CHEMBL2011264 1 7.21
CHEMBL2011244 1 7.14
CHEMBL2011430 1 7.14
CHEMBL2011435 1 7.12
CHEMBL2011261 1 7.12
CHEMBL2011260 1 7.02
CHEMBL2011247 1 7.00
CHEMBL2011248 1 6.97
CHEMBL273205 1 6.96
CHEMBL157101 KETOCONAZOLE 4.0 1 6.90
CHEMBL2011262 1 6.90
CHEMBL2011257 1 6.86
CHEMBL428780 1 6.82
CHEMBL402298 1 6.78
CHEMBL2011243 1 6.78
CHEMBL2011434 1 6.78
CHEMBL272749 1 6.67
CHEMBL2011252 1 6.61
CHEMBL2011254 1 6.61
CHEMBL2011432 1 6.57
CHEMBL2011245 1 6.50
CHEMBL402522 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL681 ETOMIDATE IC50 = 0.5 nM 9.30
CHEMBL934 METYRAPONE IC50 = 15.0 nM 7.82
CHEMBL2011431 IC50 = 16.0 nM 7.80
CHEMBL2011246 IC50 = 17.0 nM 7.77
CHEMBL2011437 IC50 = 29.0 nM 7.54
CHEMBL2011433 IC50 = 40.0 nM 7.40
CHEMBL2011253 IC50 = 42.0 nM 7.38
CHEMBL2011242 IC50 = 61.0 nM 7.21
CHEMBL2011264 IC50 = 62.0 nM 7.21
CHEMBL2011244 IC50 = 72.0 nM 7.14
CHEMBL2011430 IC50 = 73.0 nM 7.14
CHEMBL2011261 IC50 = 75.0 nM 7.12
CHEMBL2011435 IC50 = 76.0 nM 7.12
CHEMBL2011260 IC50 = 95.0 nM 7.02
CHEMBL2011247 IC50 = 101.0 nM 7.00
CHEMBL2011248 IC50 = 106.0 nM 6.97
CHEMBL273205 IC50 = 110.0 nM 6.96
CHEMBL157101 KETOCONAZOLE IC50 = 127.0 nM 6.90
CHEMBL2011262 IC50 = 126.0 nM 6.90
CHEMBL2011257 IC50 = 139.0 nM 6.86
CHEMBL428780 IC50 = 152.0 nM 6.82
CHEMBL2011434 IC50 = 167.0 nM 6.78
CHEMBL402298 IC50 = 167.0 nM 6.78
CHEMBL2011243 IC50 = 168.0 nM 6.78
CHEMBL272749 IC50 = 213.0 nM 6.67
CHEMBL2011252 IC50 = 246.0 nM 6.61
CHEMBL2011254 IC50 = 246.0 nM 6.61
CHEMBL2011432 IC50 = 269.0 nM 6.57
CHEMBL2011245 IC50 = 320.0 nM 6.50
CHEMBL402522 IC50 = 329.0 nM 6.48
CHEMBL2011255 IC50 = 362.0 nM 6.44
CHEMBL2011263 IC50 = 362.0 nM 6.44
CHEMBL2011250 IC50 = 409.0 nM 6.39
CHEMBL2011436 IC50 = 500.0 nM 6.30
CHEMBL2011241 IC50 = 500.0 nM 6.30
CHEMBL2011256 IC50 = 502.0 nM 6.30
CHEMBL2011249 IC50 = 542.0 nM 6.27
CHEMBL2010808 IC50 = 611.0 nM 6.21
CHEMBL1556445 IC50 = 663.0 nM 6.18
CHEMBL258097 IC50 = 782.0 nM 6.11
CHEMBL2011251 IC50 = 782.0 nM 6.11
CHEMBL1440486 IC50 = 816.0 nM 6.09
CHEMBL2011258 IC50 = 971.0 nM 6.01
CHEMBL2011240 IC50 = 971.0 nM 6.01
CHEMBL2011259 IC50 = 1000.0 nM 6.00
CHEMBL255759 IC50 > 1000.0 nM -